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碳青霉烯抗生素的氨基噻唑基甘氨酰衍生物。II. 含羟基吡啶酮部分的新型氨基噻唑基头孢化合物的合成与抗菌活性

Aminothiazolylglycyl derivatives of carbacephem antibiotics. II. Synthesis and antibacterial activity of novel aminothiazolyl cephem compounds with hydroxypyridone moiety.

作者信息

Mochida K, Ono Y, Yamasaki M, Shiraki C, Hirata T, Sato K, Okachi R

出版信息

J Antibiot (Tokyo). 1987 Feb;40(2):182-9. doi: 10.7164/antibiotics.40.182.

Abstract

The synthesis and antimicrobial activity of novel carbacephem antibiotics which have amido moiety of (S)-aminothiazolylglycyl side chain are described. Among them, the compound having 5-hydroxy-4-pyridon-2-carboxyl group (KT-4697) showed exceptionally strong activity against Pseudomonas aeruginosa as well as Gram-negative bacteria. A cephalosporin with this acyl group namely KT-4788 with methylpyridiniumthiomethyl group at C-3 was found to be the most active against Gram-positive and Gram-negative strains including P. aeruginosa.

摘要

描述了具有(S)-氨基噻唑基甘氨酸侧链酰胺部分的新型碳青霉烯抗生素的合成及抗菌活性。其中,具有5-羟基-4-吡啶酮-2-羧基的化合物(KT-4697)对铜绿假单胞菌以及革兰氏阴性菌显示出极强的活性。发现带有此酰基的头孢菌素,即C-3位带有甲基吡啶硫甲基的KT-4788,对包括铜绿假单胞菌在内的革兰氏阳性和革兰氏阴性菌株活性最强。

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